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A Fluorescence-Lifetime-Based Binding Assay for Class IIa Histone Deacetylases
Christian Meyners1, Monique Mertens2, Pablo Wessig2
1Fachbereich Chemie- und Biotechnologie, Hochschule Darmstadt, Haardtring 100, 64295, Darmstadt, Germany.
Chemistry (Weinheim an Der Bergstrasse, Germany)
|December 7, 2016
Summary
Researchers developed a novel binding assay for class IIa histone deacetylases (HDACs), crucial targets in diseases like cancer. This new method uses fluorescence lifetime readout, offering a robust alternative to existing enzyme activity assays for drug discovery.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Class IIa histone deacetylases (HDACs) exhibit low enzymatic activity and lack known endogenous substrates.
- These enzymes function as "Readers" of acetyl marks, mediating biological effects through protein-protein interactions.
- Class IIa HDACs are emerging pharmaceutical targets for cancer, Huntington's disease, and muscular atrophy.
Purpose of the Study:
- To develop the first binding assay for class IIa HDACs.
- To establish a robust and simple method for identifying and characterizing small-molecule ligands for class IIa HDACs.
- To provide a versatile assay applicable to other HDAC classes, such as HDAC8.
Main Methods:
- Development of a novel mix-and-measure binding assay.
- Utilized a fluorescence lifetime readout.
- Employed [1,3]dioxolo[4,5-f]benzodioxole-based ligand probes.
Main Results:
- The assay is the first of its kind for class IIa HDACs.
- It employs a simple, mix-and-measure procedure.
- The assay demonstrates a robust fluorescence lifetime readout.
Conclusions:
- The developed binding assay represents a significant advancement for studying class IIa HDACs.
- This assay provides a valuable tool for drug discovery targeting class IIa HDACs.
- The assay's principle is adaptable for other HDACs, including class I HDAC8.
